20878-56-2

Upstream product

• 118-48-9 isatoic anhydride 
• 6315-89-5 3,4-dimethoxyaniline 
• 118-92-3 anthranilic acid 
• 21563-73-5 2-aminobenzoyl chloride 

Downstream Products

• 422274-46-2 3-(3,4-dimethoxyphenyl)-2,3-dihydro-2-thioxoquinazolin-4(1H)-one 
• 312535-85-6 3-(3,4-dimethoxyphenyl)quinazolin-4(3H)-one 
• 127662-32-2 3-(3,4-Dimethoxy-phenyl)-1,2,3,4-tetrahydro-quinazoline 
• 133040-84-3 2-[2-(5-Bromo-1H-indol-3-yl)-ethyl]-3-(3,4-dimethoxy-phenyl)-3H-quinazolin-4-one 

Relevant academic research and scientific papers

New spiro pyrrole[2, 1-b]quinazolone derivative, preparation method and application thereof

The invention relates to a new spiro pyrrole[2, 1-b]quinazolone derivative, a preparation method and application thereof. The new spiro pyrrole[2, 1-b]quinazolone derivative is synthesized by using asimple method. The yield is high, the production cost is

NaNO2/I2 as an alternative reagent for the synthesis of 1,2,3-benzotriazin-4(3H)-ones from 2-aminobenzamides

An efficient transformation of 2-aminobenzamides to 1,2,3-benzotriazin-4(3H)-ones in the presence of sodium nitrite (NaNO2) and Iodine (I2) is described. The reaction is proposed to proceed via formation of nitrosyl halide that induces nitrosylation of the amino group of 2-aminobenzamide leading to diazotization followed by intramolecular cyclization.

Identification of potent orally active factor Xa inhibitors based on conjugation strategy and application of predictable fragment recommender system

Anticoagulant agents have emerged as a promising class of therapeutic drugs for the treatment and prevention of arterial and venous thrombosis. We investigated a series of novel orally active factor Xa inhibitors designed using our previously reported conjugation strategy to boost oral anticoagulant effect. Structural optimization of anthranilamide derivative 3 as a lead compound with installation of phenolic hydroxyl group and extensive exploration of the P1 binding element led to the identification of 5-chloro-N-(5-chloro-2-pyridyl)-3-hydroxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide (33, AS1468240) as a potent factor Xa inhibitor with significant oral anticoagulant activity. We also reported a newly developed Free-Wilson-like fragment recommender system based on the integration of R-group decomposition with collaborative filtering for the structural optimization process.

Natural surfactant mediated phytosynthesis and solvatochromic fluorescence of 2-aminobenzamide derivatives

A green synthesis and intriguing solvatochromic behaviour of 2-aminobenzamide derivatives in varying solvents has been investigated. The biomaterial in the form of an aqueous extract of mesocarp of the fruit of the Balanites roxburghii plant as a natural surfactant reaction medium has been employed for phytosynthesis with quantitative yield at 60 °C. The reaction proceeds effortlessly in a short reaction time with easy product formation. The fluorescence property of some synthesized compounds was studied, along with the interesting solvatochromic behaviour of 2-amino-N-benzylbenzamide.

Extending the structure-activity relationship of anthranilic acid derivatives as farnesoid x receptor modulators: Development of a highly potent partial farnesoid x receptor agonist

The ligand activated transcription factor nuclear farnesoid X receptor (FXR) is involved as a regulator in many metabolic pathways including bile acid and glucose homeostasis. Therefore, pharmacological activation of FXR seems a valuable therapeutic approach for several conditions including metabolic diseases linked to insulin resistance, liver disorders such as primary biliary cirrhosis or nonalcoholic steatohepatitis, and certain forms of cancer. The available FXR agonists, however, activate the receptor to the full extent which might be disadvantageous over a longer time period. Hence, partial FXR activators are required for long-term treatment of metabolic disorders. We here report the SAR of anthranilic acid derivatives as FXR modulators and development, synthesis, and characterization of compound 51, which is a highly potent partial FXR agonist in a reporter gene assay with an EC50 value of 8 ± 3 nM and on mRNA level in liver cells.

Convenient and sequential one-pot route for synthesis of 2-thioxoquinazolinone and quinazolinobenzothiazinedione derivatives

A new and efficient synthetic process has been developed for preparation of 2-thioxoquinazolinone and quinazolinobenzothiazinedione derivatives. The related products were synthesized through reaction of isatoic anhydride, amines/anthranilic acids, and carbon disulfide (CS2) in the presence of potassium hydroxide in ethanol at reflux. Graphical abstract: [Figure not available: see fulltext.]

Synthesis and in vitro study of platelet antiaggregant activity of 1,2,3,4-tetrahydroquinazoline derivatives

Some original 3-substituted 1,2,3,4-tetrahydroquinazolines were synthesized. Their antiplatelet activity was evaluated in vitro with respect to aggregation induced by the main inducers (ADP, collagen, arachidonic acid), platelet serotonin release reaction and thromboxane A2 synthesis. All these molecules possess an inhibiting power which, compared to that of aspirin in the same conditions, is the same or greater when aggregation is induced by ADP.